Inhibitors Product Data Sheet

Epelsiban • Agonists

Cat. No.: HY-105018 CAS No.: 872599-83-2

Molecular Formula: C₃₀H₃₈N₄O₄ •

Molecular Weight: 518.65 Screening Libraries Target: Oxytocin Receptor Pathway: GPCR/G Protein Storage: Please store the product under the recommended conditions in the Certificate of Analysis.

BIOLOGICAL ACTIVITY

Description Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.

IC₅₀ & Target pKi: 9.9 (human oxytocin receptor)[1] IC50: 192 nM (human oxytocin receptor)[1]

In Vitro Epelsiban is a potent oxytocin receptor, with a pKi of 9.9 for human oxytocin receptor, >31000-fold selectivity over all three human vasopressin receptors hV1aR (pKi, <5.2), hV2R (pKi, <5.1), and hV1bR (pKi, 5.4), and shows no significant P450 inhibition[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo Epelsiban shows an IC50 of 192 nM for oxytocin receptor in rats. Epelsiban has low levels of intrinsic clearance against the microsomes of rat, dog, and cynomolgus monkey, good bioavailability (55%), but is negative in the genotoxicity screens with a satisfactory oral safety profile in female rats[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

REFERENCES

[1]. Borthwick AD, et al. Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency. J Med Chem. 2012 Jan 26;55(2):783-96.

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Caution: Product has not been fully validated for medical applications. For research use only. Tel: 609-228-6898 Fax: 609-228-5909 E-mail: [email protected] Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA

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